2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors |
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Authors: | Moravec Jirí Krystof Vladimír Hanus Jan Havlícek Libor Moravcová Daniela Fuksová Kvetoslava Kuzma Marek Lenobel René Otyepka Michal Strnad Miroslav |
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Affiliation: | Isotope Laboratory, Institute of Experimental Botany, Academy of Sciences of the Czech Republic, Vídenská 1083, 14220 Prague 4, Czech Republic. |
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Abstract: | Purine inhibitors of cyclin-dependent kinases attract attention as potential anticancer drugs because their first representative roscovitine recently entered clinical trials. Although well described in terms of structure-activity relationships, we still present here a novel modification of the purine scaffold influencing their inhibitory properties. The introduced C-8 substituents, however, lowered the CDK inhibitory activity of roscovitine, whereas the antiproliferative potential of several derivatives remained high. |
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